R788(Fostamatinib disodium)

Bezeichnung:R788(Fostamatinib disodium)

CAS-Nr1025687-58-4

Englisch Name:R788(Fostamatinib disodium)

CBNumberCB32518272

SummenformelC23H27FN6NaO9P

Molgewicht604.46

MOL-Datei1025687-58-4.mol

R788(Fostamatinib disodium) physikalisch-chemischer Eigenschaften

Schmelzpunkt	>191°C (dec.)
storage temp.	Store at -20°C
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
Aggregatzustand	Solid
Farbe	Off-White
Stabilität	Hygroscopic

R788(Fostamatinib disodium) Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
R 788 Sodium Salt is the sodium salt of R 788 which is a selective spleen tyrosine kinase (Syk) inhibitor. It may be used in the treatment of autoimmune diseases such as type 1 diabetes and has been tested in the treatment of rheumatoid athritis, leukemia and lymphoma.
Biologische Aktivität
r788, which is the prodrug of r406, is a potnet and selective syk inhibitor. the spleen tyrosine kinase (syk) plays a key role in the signaling of activating fc receptors and the b-cell receptor (bcr).
in vitro
r406 was found to induce the apoptosis of the majority of examined dlbcl cell lines and could specifically inhibit both tonic- and ligand-induced bcr signaling (autophosphorylation of syk525/526 and sykdependent phosphorylation of the b-cell linker protein [blnk]) [1].
in vivo
r788 effectively inhibits bcr signaling, demonstrating reduced proliferation and survival of the malignant b cells and significantly prolonged survival of the treated eμ-tcl1 transgenic mouse. moreover, the effect of r788 was found to be selective for the malignant clones, since no disturbance in the production of normal b lymphocytes was observed [2].
target
Syk
Einzelnachweise
[1] chen l, monti s, juszczynski p, daley j, chen w, witzig te, habermann tm, kutok jl, shipp ma. syk-dependent tonic b-cell receptor signaling is a rational treatment target in diffuse large b-cell lymphoma. blood. 2008 feb 15;111(4):2230-7.
[2] suljagic m, longo pg, bennardo s, perlas e, leone g, laurenti l, efremov dg. the syk inhibitor fostamatinib disodium (r788) inhibits tumor growth in the eμ- tcl1 transgenic mouse model of cll by blocking antigen-dependent b-cell receptor signaling. blood. 2010 dec 2;116(23):4894-905.
[3] bajpai m. fostamatinib, a syk inhibitor prodrug for the treatment of inflammatory diseases. idrugs. 2009 mar;12(3):174-85.

R788(Fostamatinib disodium) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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